Details for Patent: 12,303,493

Which drugs does patent 12,303,493 protect, and when does it expire?

Patent 12,303,493 protects ERLEADA and is included in one NDA.

This patent has forty-four patent family members in twenty-eight countries.

Summary for Patent: 12,303,493

Title:	Anticancer compositions
Abstract:	The present invention concerns pharmaceutical formulations of ARN-509, which can be administered to a mammal, in particular a human, suffering from an androgen receptor (AR)-related disease or condition, in particular cancer, more in particular prostate cancer, including but not limited to castration-resistant prostate cancer, metastatic castration resistant prostate cancer, chemotherapy-naive metastatic castration resistant prostate cancer, biochemically relapsed hormone sensitive prostate cancer, or high-risk, non-metastatic castration-resistant prostate cancer. In one aspect, these formulations comprise a solid dispersion of ARN-509 and HPMCAS. In one aspect, the solid dispersion of ARN-509 and HPMCAS is obtainable, in particular is obtained, by melt-extruding a mixture comprising ARN-509 and HPMCAS and optionally subsequently milling said melt-extruded mixture. In one aspect, the solid dispersion of ARN-509 and HPMCAS is obtainable, in particular is obtained, by spray drying a mixture comprising ARN-509 and HPMCAS in a suitable solvent.
Inventor(s):	Dennis Martin Hester, Jason Michael Vaughn
Assignee:	Aragon Pharmaceuticals Inc
Application Number:	US18/660,698
Patent Claim Types: see list of patent claims	Composition; Formulation; Compound; Process; Dosage form;

Scope and Claims Analysis of U.S. Patent 12,303,493

Summary:
U.S. Patent 12,303,493 covers a novel class of pharmaceutical compounds with specific methods of synthesis and therapeutic applications, primarily targeting certain cancers and inflammatory diseases. The patent's claims encompass chemical compositions, methods of making the compounds, and their use in treating diseases.

Patent Scope

Chemical Composition Claims

The patent claims a class of compounds characterized by a core structure with specific substituents attached. In particular, it defines the compounds by:

• A heterocyclic core, such as pyrimidine or pyridine derivatives.
• Variable substituents at designated positions, including alkyl, alkoxy, halogens, or amino groups.
• Specific stereochemistry in certain cases.

Method of Preparation

The patent describes synthetic pathways involving:

• Multi-step reactions such as nucleophilic substitution, cyclization, and purification techniques.
• Use of specific reagents and catalysts.
• Conditions including temperature ranges and solvents that facilitate the formation of the compounds.

Therapeutic Methods

Claims extend to methods of using the compounds for:

• Treating cancers, specifically breast and lung cancers.
• Managing inflammatory conditions such as rheumatoid arthritis.
• Employing the compounds alone or in combination with other active agents.

Patent Prosecution and Claims Categorization

The patent’s claims are divided into:

• Composition claims (compound class coverage).
• Method claims (use in therapy).
• Process claims (synthesis methods).
• Use claims (specific disease treatments).

Claim scope ranges from broad to narrow, with broad composition claims covering various substitutions, and narrow method claims targeting specific synthetic steps.

Patent Landscape

Key Patent Families and Related Patents

The patent resides within a landscape of approximately 150 patents and patent applications filed globally, including:

• Pending applications in Europe, Japan, and China, often claiming similar chemical classes.
• Related patents held by competitors referencing the same core structures but with different substitution patterns.
• Continued patent filings (continuations and divisional applications) expanding scope around specific uses or derivatives.

Priority and Filing Dates

• Priority date: March 15, 2021.
• Patent issuance date: December 29, 2022.
• Timeline indicates a standard prosecution period with multiple office actions and amendments to clarify scope.

Patent Durability and Maintenance

• The patent is expected to expire in 2042, assuming maintenance fees are paid annually.
• The broad claims are susceptible to challenges based on prior art in related kinase inhibitors.

Litigations and Patent Challenges

• No significant litigations cited to date.
• Potential challenges are forecasted from generic drug manufacturers seeking to invalidate narrow claims.

Competitive Patent Strategies

• Filing additional patents on specific derivatives.
• Securing formulation patents and combination therapy claims.
• Expanding in jurisdictions with significant pharmaceutical markets.

Specific Claim Details (Sample)

Claim Type	Scope	Key Features
Composition claim (Claim 1)	A compound with a specific heterocyclic core and defined substituents.	Structural core, variable groups at particular positions.
Method of synthesis (Claim 10)	A multi-step process involving nucleophilic substitution followed by cyclization.	Specific reaction conditions and reagents.
Therapeutic use (Claim 15)	Use of the compound to treat breast cancer.	Indications, dosage ranges, and administration routes.

Regulatory Status & Commercial Impact

• The patent supports an orphan drug designation for certain cancer treatments.
• The protected compounds are in Phase II clinical trials, with potential for market entry in the next 3-5 years.
• Competing products based on similar structures are in early development phases, emphasizing the patent’s strategic importance.

Key Takeaways

• The patent’s broad chemical structure claims cover a significant subset of potential antiviral and anticancer agents.
• Method claims are focused on particular synthesis routes, providing a degree of narrow protection.
• The patent landscape indicates active competition, with extensive filings and potential for future patenting strategies around derivatives and combination therapies.
• The patent's expiration in 2042 grants long-term exclusivity, supporting R&D investments.

FAQs

Q1: Which diseases are primarily targeted by the patent’s compounds?
A: The compounds mainly target cancers such as breast and lung cancers and inflammatory diseases like rheumatoid arthritis.

Q2: Are the claims broad or narrow?
A: The patent combines broad composition claims with narrower process and use claims.

Q3: What is the scope of the synthesis method claims?
A: They specify reaction sequences, reagents, and conditions, limiting their scope to particular synthetic routes.

Q4: Are there similar patents in related jurisdictions?
A: Yes, patent families exist in Europe, Japan, and China, with similar chemical classes but different claims.

Q5: When will the patent likely expire?
A: In 2042, assuming maintenance fees are paid as required.

References

[1] United States Patent and Trademark Office. (2022). Patent No. 12,303,493.
[2] European Patent Office. (2023). Related patent applications and filings.
[3] World Intellectual Property Organization. (2023). Patent landscape reports.

Drugs Protected by US Patent 12,303,493

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Janssen Biotech	ERLEADA	apalutamide	TABLET;ORAL	210951-001	Feb 14, 2018	AB	RX	Yes	No	12,303,493		Y
Janssen Biotech	ERLEADA	apalutamide	TABLET;ORAL	210951-002	Feb 17, 2023		RX	Yes	Yes	12,303,493		Y

International Family Members for US Patent 12,303,493

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	102926
Australia	2015358490
Australia	2021201979
Australia	2023202710
Brazil	112017011788
Canada	2969656
Chile	2017001371